36273-89-9Relevant academic research and scientific papers
Carbazole-based semicarbazones and hydrazones as multifunctional anti-Alzheimer agents
Chaudhary, Bharat N.,Gandhi, Bhumi,Kanhed, Ashish M.,Patel, Dushyant V.,Patel, Kirti V.,Patel, Kishan B.,Patel, Nirav R.,Prajapati, Navnit K.,Shah, Bhavik S.,Teli, Divya M.,Yadav, Mange Ram
, (2021/07/14)
With the aim to combat a multi-faceted neurodegenerative Alzheimer’s disease (AD), a series of carbazole-based semicarbazide and hydrazide derivatives were designed, synthesized and assessed for their cholinesterase (ChE) inhibitory, antioxidant and biometal chelating activity. Among them, (E)-2-((9-ethyl-9H-carbazol-3-yl)methylene)-N-(pyridin-2-yl)hydrazinecarbothioamide (62) and (E)-2-((9-ethyl-9H-carbazol-3-yl)methylene)-N-(5-chloropyridin-2-yl)hydrazinecarbothioamide (63) emerged as the premier candidates with good ChE inhibitory activities (IC50 values of 1.37 μM and 1.18 μM for hAChE, IC50 values of 2.69 μM and 3.31 μM for EqBuChE, respectively). All the test compounds displayed excellent antioxidant activity (reduction percentage of DPPH values for compounds (62) and (63) were 85.67% and 84.49%, respectively at 100 μM concentration). Compounds (62) and (63) conferred specific copper ion chelating property in metal chelation study. Molecular docking studies of compounds (62) and (63) indicate strong interactions within the active sites of both the ChE enzymes. Besides that, these compounds also exhibited significant in silico drug-like pharmacokinetic properties. Thus, taken together, they can serve as a starting point in the designing of multifunctional ligands in pursuit of potential anti-AD agents that might further prevent the progression of ADs. Communicated by Ramaswamy H. Sarma.
CHEMICAL ACTIVATORS OF NICOTINAMIDE MONONUCLEOTIDE ADENLYLY TRANSFERASE 2 (NMNAT2) AND USES THEREOF
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Page/Page column 23; 29-30, (2020/06/22)
The present application relates to novel semicarbazones and thiosemicarbazones, to processes for preparing them, to pharmaceutical preparations comprising them, to the use of the novel semicarbazones and thiosemicarbazones for treatment and/or prophylaxis of diseases and to the use thereof for production of a medicament for treatment and/or prophylaxis of diseases, especially of neurodegeneration and age-associated diseases or conditions associated with NAD loss. The present application also provides a method for high throughput screening of NMNAT2 activators.
5-Nitrofuran-2-yl derivatives: Synthesis and inhibitory activities against growing and dormant mycobacterium species
Sriram, Dharmarajan,Yogeeswari, Perumal,Dhakla, Prathiba,Senthilkumar, Palaniappan,Banerjee, Debjani,Manjashetty, Thimmappa H.
body text, p. 1152 - 1154 (2009/08/07)
Eighteen 5-nitrofuran-2-yl derivatives were prepared by reacting 5-nitro-2-furfural with various (sub)phenyl/pyridyl thiosemicarbazide using microwave irradiation. The compounds were tested for their in vitro activity against tubercular and various non-tubercular mycobacterium species in log-phase and 6-week-starved cultures. Compound N-(3,5-dibromopyridin-2-yl)-2-((5-nitrofuran-2-yl)methylene)hydrazinecarbothioamide (4r) was found to be the most potent compound (MIC: 0.22 μM) and was 3 times more active than standard isoniazid (INH) and equally active as rifampicin (RIF) in log-phase culture of Mycobacterium tuberculosis H37Rv. In starved M. tuberculosis H37Rv, 4r inhibited with MIC of 13.9 μM and was found to be 50 times more active than INH and slightly more active than RIF.
Platinum (IV) thiohydrazide, thiodiamine and thiohydrazone complexes: A spectral, antibacterial and cytotoxic study
Mishra,Mishra,Manav,Kumar,Sharad,Chandra,Saluja,Kaushik
, p. 1042 - 1047 (2008/02/03)
Some platinum (IV) complexes [Pt(L)2Cl2] [where, L = 2-aminopyridine-N-thiohydrazide (L1), (2-aminopyridine-N-thio)-1,3-propanediamine (L2), benzaldehyde-2-aminopyridine-N-thiohydrazone (L3) and salicylaldehyde-2-aminopyrtidine-N-thiohydrazone (L4)] have been synthesized. The thiohydrazides, thiodiamine and thiohydrazones can exist as thione-thiol tautomer and coordinate as a bidentate N-S ligand. The ligands found to act in monobasic bidentate fashion. Analytical data reveals that metal to ligand stoichiometry is 1:2. The complexes have been characterized by elemental analysis, IR, mass, electronic and 1H NMR spectroscopic studies. In vitro antibacterial and cytotoxic study have also been carried out for some complexes.
Synthesis and glucose-6-phosphatase inhibitory activity of (thiouriedo)alkanoic acid esters
Farhanullah,Sil, Diptesh,Tripathi, Brajendra K.,Srivastava, Arvind K.,Ram, Vishnu Ji
, p. 2571 - 2574 (2007/10/03)
A series of (3-pyridin-2-yl-thiouriedo)alkanoic acid esters (5a-j) have been synthesized by the reaction of pyridin-2-yl-dithiocarbamic acid methyl ester (2) and amino acid esters (4). Most of the synthesized compounds have been evaluated against glucose-6-phosphatase enzyme but only four compounds (5g-j) displayed significant inhibitory activity of the enzyme.
Herbicidal 1-pyridyltetrazolinones
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, (2008/06/13)
Herbicidal tetrazolinone derivatives of the formula: STR1 in which R1 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl or phenyl, and R2 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl or phenyl, or R1 and R2 together with the nitrogen atom to which they are bonded form an optionally benzofused heterocyclic ring, which is optionally substituted by C1-4 alkyl, n is 0, 1, 2 or 3, and R3 each independently is nitro, halogen, alkyl, haloalkyl, alkylthio or phenoxy.
